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Anesthesia Pharm (A) > Opioid Agonist-Antagonists (2) > Flashcards

Opioid Agonist-Antagonists (2) Flashcards

1
Q

When are opioid agonist-antagonists used?

A

Used if unable to tolerate a pure agonist

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2
Q

What receptors do opioid agonist-antagonists bind to?

A

Mu receptors: Partial effect (agonist) not no effect (competitive antagonist)

Kappa/Delta receptors: Partial effect (agonist)

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3
Q

What are generalized side effects of opioid agonst-antagonists?

A

Same as opioids + dysphoric reactions (stress/uneasiness)

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4
Q

What are advantages of opioid agonist-antagonists?

A
  • Analgesia
  • Limited depression of ventilation
  • Low potential for dependence
  • Ceiling effect prevents additional responses
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5
Q

What is the ceiling effect for opioid agonist-antagonists?

A

Drugs impact on body plateaus→ taking higher doses does not increase its effect

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6
Q

List opioid agonist-antagonists from most potent to least potent when compared to morphine:

A
  • Buprenorphine (50x more)
  • Butorphanol (4x more)
  • Bremazocine (2x more)
  • Nalbuphine (equal)
  • Nalorphine (equal)
  • Dezocine
  • Pentazocine (1/5)
  • Meptazinol
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7
Q

What is the primary MOA of Pentazocine?

A

Agonist effects on delta and kappa
Weak antagonist activity

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8
Q

What med antagonizes Pentazocine?

A

Naloxone

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9
Q

How is Pentazocine metabolized and excreted?

A
  • Extensive hepatic first pass
  • Excreted in urine (glucuronide conjugates)
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10
Q

Chronic pain dose of Pentazocine:

A

10-30 mg IV or 50mg PO

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11
Q

What dose of Pentazocine causes analgesia sedation and depression of ventilation?

A

20-30 mg IM

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12
Q

How does epidural duration of action of pentazocine compare to morphine?

A

Shorter duration of action compared to morphine

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13
Q

What are side effects of Pentazocine?

A

Sedation
↑HR, BP, PAP, LVEDP
Diaphoresis
Dizziness

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14
Q

Does Pentazocine cross placental barrier?

A

Yes, Causes fetal depression

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15
Q

How does Butorphanol compare to Pentazocine?

A

Butorphanol 20X agonist effect and 10-30x antagonist effect than Pentazocine

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16
Q

Which receptors does Butorphanol have affinity for?

A

Mu receptor → Low affinity
Kappa receptor → Moderate affinity
Sigma receptor → Minimal affinity

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17
Q

2-3 mg IM Butorphanol= ____ mg Morphine

A

10

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18
Q

T/F: IM Butorphanol has less absorption.

A

False: Butorphanol is rapidly and completely absorbed with IM admin

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19
Q

What is the E1/2 time for Butorphanol?

A

2.5-3.5 hrs

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20
Q

How is Butorphanol metabolized/eliminated?

A
  • Hepatic metabolism
  • Eliminated largely in bile
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21
Q

What are side effects of Butorphanol?

A
  • Sedation
  • Nausea
  • Diaphoresis
  • Withdrawal symptoms
  • ↑ BP, PAP, CO
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22
Q

_________ stops post op shivering more effectively than other opioids.

A

Butorphanol: Has more kappa effects

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23
Q

_________ is useful in the treatment of chronic pain when there is a high risk of physical dependence.

A

Pentazocine

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24
Q

It may be difficult to use an opioid agonist affectively as an analgesic in the presence of _____________.

A

Butorphanol

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25
Q

Which receptors has a moderate affinity for Butorphanol effects to mitigate shivering and produce analgesia?

A

Kappa receptor

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26
Q

What is the E1/2 time for Nalbuphine?

A

3-6 hours

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27
Q

What is used to reverse the agonist effects of nalbuphine?

A

Naloxone

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28
Q

Which receptors does Nalbuphine act as an agonist? How does the agonist activity compare with morphine?

A

Mu: equally as potent as morphine

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29
Q

How does Nalbuphine antagonist effects compare to Nalorphine?

A

1/4 as potent as Nalorphine

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30
Q

What is E1/2 time for Nalbuphine? Where is it metabolized?

A

E1/2: 3-6 hrs
Metabolized in the liver

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31
Q

What are side effects of Nalbuphine?

A
  • Sedation
  • Dysphoria
  • Withdrawal symptoms
    ** NO increase in BP, PA, HR or atrial filling
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32
Q

Which opioid agonist-antagonist would be best to use for cardiac cath patients?

A

Nalbuphine

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33
Q

Which opioid agonist-antagonist has agonist affects 50X more potent than morphine?

A

Buprenorphine

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34
Q

Which receptors does Buprenorphine bind to?

A

Mu receptors agonist

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35
Q

What is the onset for Buprenorphine?

A

30 min

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36
Q

What is the duration of Buprenorphine?

A

8 hours (prolonged resistance to Naloxone)

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37
Q

When is Buprenorphine used?

A

Post op, cancer, renal colic, and MI; epidural

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38
Q

What are side effects of Buprenorphine?

A
  • Drowsiness
  • N/V
  • Vent depression
  • Pulm edema
  • Withdrawal
  • Low risk for abuse
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39
Q

0.3mg IM Buprenorphine is ____X more potent than morphine

A

50X

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40
Q

What is the only clinically used opioid that has higher affinity of the mu receptor than Buprenorphine?

A

Sufentanil

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41
Q

Which opioid agonist-antagonist (not in practice) is equally as potent as morphine but has a high incidence of dysphoria?

A

Nalorphine

42
Q

Which opioid agonist-antagonist is 2x more potent than morphine by working on the kappa receptors?

A

Bremazocine

43
Q

Which opioid agonist-antagonist work on delta and mu receptors to provide analgesia with no CV effects?

44
Q

Which receptor does Meptazinol bind to? What is the onset and duration?

A

Mu1 receptors

Rapid onset
<2 hour duration
Protein binding 25%

45
Q

What is the onset of Dezocine?

46
Q

Which receptor do opioid antagonists bind to? What are these drugs?

A
  • Pure Mu opioid receptor antagonists
  • Naloxone, Naltrexone, Nalmefene
47
Q

What is the MOA of opioid antagonists?

A

Competitive antagonist: high affinity to opioid receptors (bumps opioid off and binds to receptor but doesnt activate it)

48
Q

Which opioid antagonist is nonselective with all 3 opioid receptors?

49
Q

What are the uses for Naloxone?

A
  • Opioid-induced depression postop
  • Neonate depression (from mom)
  • Opioid OD
  • Detect dependence
  • Hypovolemic/septic shock
  • Antagonism of GA (high doses)
50
Q

What is the dose for Naloxone? What is the continuous gtt dose?

A

1- 4 mcg/kg IV
5 mcg/kg IV infusion

51
Q

What is the dose of naloxone for shock? How much Naloxone can be given for epidural side effects?

A

Shock: >1 mg/kg IV
Epidural side effects: 0.25 mcg/kg/hr IV

52
Q

What is the duration of Naloxone?

53
Q

What is the E1/2 time for Naloxone?

A

60-90 minutes

54
Q

What are side effects of Naloxone?

A

Reversal of analgesia (intended)
N/V (give slow IVP)
Increase SNS (HR, BP, pulm edema, cardiac dysrhythmias)

55
Q

What route does Naltrexone have the most effect?

56
Q

What is the duration of Naltrexone?

57
Q

What is Naltrexone used for?

A

Alcoholism

58
Q

How does Nalmefene potency compare to Naloxone? What is the dose?

A

Equipotent
15- 25 mcg IV (every 2-5 min) (1mcg/kg)

59
Q

What is the E1/2 time for Nalmefene?

60
Q

What are the clincal uses for Methylnalrexone?

A

Promotes gastric emptying and antagonizes N/V

61
Q

Methylnaltrexone is highly ionized (quaternary). What does this mean?

A

Quaternary limits crossing of BBB (better for periphery)

No alteration is centrally mediated analgesia

62
Q

What are uses for Alvimopan?

A

Post op ileus (increases peristalsis)

63
Q

What is a newer mu selective PO peripheral opioid antagonist?

64
Q

What are the limitations to the uses of Alvimopan?

A

Not for long term use (could cause CV events)

65
Q

Metabolism of Alvimopan relies on _____ _______.

66
Q

What is the strategy for making tamper/abuse resistance opioids?

A

Combining opioid with antagonist (ex: Suboxone, Embeda, Oxynal)

67
Q

What are the components of Suboxone, Embeda, and OxyNal?

A

Suboxone: Buprenorphine + Naloxone
Embeda: (ER morphine + Naltrexone)
OxyNal: Oxycodone+ Naltrexone

68
Q

Is it common to have opioid allergy?

A

No, True opioid allergy is rare

Predictable side effects like localized histamine release are misinterpreted as allergies

69
Q

How might opioid therapy potentially alter immunity?

A

Through Neuroendocrine effects or via direct effects on immune system (with prolonged opioid exposure)

Opioid receptors are present in B and T cells, dendritic cells, neutrophils

71
Q

Sufentanil decreases MAC with Enflurane by ___ - ___%

72
Q

Alfentanil decreases MAC up to ___%

73
Q

Remifentanil decreases MAC ___ -____%

74
Q

Which opioid agonist-antagonist has the highest decrease in MAC when used in combo with volatile anesthetics?

A

Pentazocine (20% decrease in MAC)

75
Q

Is MAC affected by Opioid agonist-antagonists?

A

Butorphanol (11% decrease)
Nalbuphine (8% decrease)

76
Q

What are the suggested starting IV regimens of PCA for Morphine, Hydropmorphone, and Fentanyl?

77
Q

Why PCA over PRN drug dosing for pain management?

A

After achieving effective concentrations, PCA allows patients to self titrate opioid dosing to maintain effective analgesia

No lag time between request for pain med and nurse getting/giving (minimizing time in pain with easy access from PCA)

78
Q

What meds minimize pain perception in the brain through DIC?

A

Opioids, Alpha 2 agonists ,General anesthetics

79
Q

Which meds work to minimize pain through modulation of afferent signals in the spinal cord?

A

LA, Opioids, Ketamine, alpha2 agonists

80
Q

Which meds minimize pain transmission by A delta and C fibers?

A

Local anesthetics

81
Q

Which meds reduce pain by limiting pain transduction by peripheral nociceptors?

A

LA, NSAIDS

82
Q

Where are opioid receptors in the spinal cord located?

A

Substantia gelatinosa

83
Q

What does Neuraxial mean?

A

Below the brain

84
Q

How are neuraxial opioids given?

A

Either epidural or spinal

85
Q

How is epidural opioid different from spinal/SAB opioids?

A
  • Epidural dose is increased 5-10 times
  • Systemic absorption of drug
86
Q

What does the addition of Epi to the solution places into the epidural space do?

A

Decreases systemic absorption of the opioid–enhances post op analgesia

Add vasoconstrictor (Epi)

87
Q

How the lipid solubility differ between epidural admin of Fentanyl, Morphine, and Sufentanil? what is the peak in the CSF

A

Sufentanil: Most lipid soluble (1600x >morphine) peak in 6 min

Fentanyl (800x > morphine) peak 20 min

Morphine: slower onset, longer duration. peak 1-4 hrs

88
Q

What is Cephalad movement in CSF and what is this dependent on?

A

Movement upward (toward the head)

Depends on lipid solubility of drug

89
Q

Which has the most and least cephalad migration: Fent, Morphine. Sufen?

A
  • Fentanyl and Sufentanil: highly lipid soluble are limited in cephalad migration d/t rapid uptake in the spinal cord
  • Morphine: less lipid soluble remains in CSF longer and can go to more cephalad locations
90
Q

What can increase movement for CSF?

A

Coughing or straining

91
Q

Why does the barocity of med matter?

A

Baracity is the density of the med

Hyperbaric: Med sinks
Hypobaric: Med floats
Isobaric: remains at same level

92
Q

What LA anesthetic baracity would affect right hip of a patient positioned in left lateral position?

A

Hypobaric LA

93
Q

What are the CSF and plasma peak times as well as cervical levels in epidural fentanyl, Sufentanil, and morphine?

94
Q

What puts patient at high risk for hypotension and bradycardia following spinal anesthesia?

A

Anesthesia above T5
(T1-T4= cardiac accelerators)

95
Q

Common side effects from neuraxial opioids (dose dependent):

A

Pruritus (most common in face, neck, upper thorax in OB)
N/V
Urinary retention
Vent depression
Sedation
CNS Excitation

96
Q

What is the cause of Neuraxial opioid pruritus? What is the treatment?

A

Cephalad migration to trigeminal nucleus (brainstem)

TX: naloxone, Antihistamines, gabapentin

97
Q

What is the most reliable sign of depression of ventilation post Neuraxial opioid admin?

A

Early: within 2 hours (d/t systemic absorption)
Late: 6-12 hours after (d/t cephalad migration of opioid in CSF to ventral medulla)

Depressed LOC secondary to hypercarbia (late sign)

98
Q

What is the treatment of depressed ventilation after spinal opioid?

A

Naloxone: 0.25 mcg/kg/hr IV

99
Q

What does CNS excitation S/E from spinal opioid look like?

A

Tonic skeletal muscle rigidity ike seizure activity

100
Q

What adverse effect can happen 2-5 days after epidural opioid?

A

Herpes simplex labialis viral reactivity: (likely d/t cephalad migration of opioid CSF and interaction with trigeminal nucleus)

101
Q

Should neuraxial opioids be withheld from women recovering from cesarean delivery d/t concern for neonatal drug exposure in breast milk?

A

No, Concentration of opioid in breastmilk is negligible after neuraxial opioids

Anesthesia Pharm (A) (17 decks)

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